LEUPEPTIN HEMISULFATE MONOHYDRATE
LEUPEPTIN HEMISULFATE MONOHYDRATE Basic information
- Product Name:
- LEUPEPTIN HEMISULFATE MONOHYDRATE
- Synonyms:
-
- (s)-2-(2-acetamido-4-methylvaleramido)-n-(1-formyl-4-guanidinobutyl)-4-methy
- l-valeramide
- methyl-(s)-
- LEUPEPTIN HEMISULFATE MONOHYDRATE
- 6-O-B-D-GLUCOPYRANOSYL-D-GLUCOPYRANOSE
- Ac-Leu-Leu-Arg-aldehyde . sulfate
- Gentibiose
- (2S)-2-[(Ac-Leu-Leu-)Amino]-5-guanidinopentanal
- CAS:
- 55123-66-5
- MF:
- C20H38N6O4
- MW:
- 426.55
- Product Categories:
-
- Antibiotics
- Mol File:
- 55123-66-5.mol
LEUPEPTIN HEMISULFATE MONOHYDRATE Chemical Properties
- Boiling point:
- 541.98°C (rough estimate)
- Density
- 1.1865 (rough estimate)
- refractive index
- 1.6000 (estimate)
- RTECS
- YV4205100
- pka
- 13.44±0.46(Predicted)
- form
- Powder
LEUPEPTIN HEMISULFATE MONOHYDRATE Usage And Synthesis
Uses
Leupeptin is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin potently inhibits serine, cysteine and threonine proteases. Leupeptin inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity[1][2][3].
Definition
ChEBI: Leupeptin is a tripeptide composed of N-acetylleucyl, leucyl and argininal residues joined in sequenceby peptide linkages. It is an inhibitor of the calpains, a family of calcium-activated proteases which promote cell death. It has a role as a serine protease inhibitor, a bacterial metabolite, a cathepsin B inhibitor, a calpain inhibitor and an EC 3.4.21.4 (trypsin) inhibitor. It is a tripeptide and an aldehyde. It is a conjugate base of a leupeptin(1+).
Safety Profile
Questionable carcinogen withexperimental neoplastigenic data. When heated todecomposition it emits toxic fumes of NOx.
in vivo
Leupeptin (0, 9, 18, 36 mg/kg; i.p.; single) is well tolerated by the animals and produces a strong, dose-dependent increase in LC3b-II in both the total tissue extracts and the lysosome and autophagosome-enriched pellet fraction[2].
| Animal Model: | C57BL/6NCrl male mice (6-8 weeks old, 20-25 g)[1]. |
| Dosage: | 0, 9, 18, 36 mg/kg |
| Administration: | Intraperitoneal injection; single |
| Result: | Promoted the accumulation of LC3b-II in mouse liver. |
References
[1] Aoyagi T, et al. Biological activities of leupeptins. J Antibiot (Tokyo). 1969 Nov;22(11):558-68. DOI:10.7164/antibiotics.22.558
[2] Fu L, et al. Mechanism of Microbial Metabolite Leupeptin in the Treatment of COVID-19 by Traditional Chinese Medicine Herbs. mBio. 2021 Oct 26;12(5):e0222021. DOI:10.1128/mBio.02220-21
[3] Haspel J, et al. Characterization of macroautophagic flux in vivo using a leupeptin-based assay. Autophagy. 2011 Jun;7(6):629-42. DOI:10.4161/auto.7.6.15100
[4] Aoyagi T, et al. Biological activities of leupeptins. J Antibiot (Tokyo). 1969 Nov;22(11):558-68.
LEUPEPTIN HEMISULFATE MONOHYDRATESupplier
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LEUPEPTIN HEMISULFATE MONOHYDRATE(55123-66-5)Related Product Information
- N-ETHYLGUANIDINIUM SULFATE
- (S)-Propane-1,2-diamine sulfate
- ETHYLENEDIAMINE SULFATE
- Mafenide hydrochloride
- Milacemide
- 1-METHYLGUANIDINE SULFATE
- H-LEU-NH2
- Agmatine sulfate
- Guanidine sulfate
- Leupeptin
- LEUPEPTIN
- AC-GLY-LEU-NH2
- PROPIONYL-LEU-LEU-ARG-AL HEMISULFATE
- AC-LEU-NHME
- AC-LEU-NH2
- N-ACETYLPUTRESCINE HYDROCHLORIDE
- LEUPEPTIN HEMISULFATE MONOHYDRATE
- N-(2-aminoethyl)butane-1,4-diamine